抑肽酶作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetAprotininCat. No.: HY-P0017CAS No.: 9087-70-1分式: CHNOS分量: 6511.44Sequence: Arg-Pro-Asp-Phe-Cys-Leu-Glu-Pro-Pro-Tyr-Thr-Gly-Pro-Cys-Lys-Ala-Arg-Ile-Ile-Arg-Tyr-Phe-Tyr-Asn-Ala-Lys-Ala-Gly-Leu-Cys-Gln-Thr-Phe-Val-Tyr-Gly-Gly-Cys-Arg-Ala-Lys-Arg-Asn-Asn-Phe-Lys-Ser-Ala-Glu-Asp-Cys-Met

2、-Arg-Thr-Cys-Gly-Gly-AlaSequence Shortening: RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA作靶點: Influenza Virus作通路: Anti-infection儲存式: Powder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 100 mg/mL (15.36 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentr

3、ation制備儲備液1 mM 0.1536 mL 0.7679 mL 1.5358 mL5 mM 0.0307 mL 0.1536 mL 0.3072 mL10 mM 0.0154 mL 0.0768 mL 0.1536 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。BIOLOGICAL ACTIVITY物活性 Aprotinin 分離肺的絲氨酸蛋酶 (BPTI) 抑制劑，對胰

4、蛋酶和胰凝乳蛋酶胰凝乳蛋酶的 Ki 值分別為0.06 pM和9 nM。IC & Target Ki: 0.06 pM (Trypsin), 9 nM (Chymotrypsin)1體外研究Aprotinin, a serine protease inhibitor isolated from bovine lung, is a complex protease inhibitor that is anPage 1 of 2 www.MedChemEantifibrinolytic, inhibits contact activation, and decreases the inflammat

5、ory response to cardiopulmonary bypass2.Aprotinin inhibits trypsin (bovine, Ki= 0.06 pM), chymotrypsin (bovine, Ki= 9 nM), plasmin (human, 0.23 nM)1.Aprotinin is also a competitive protein inhibitor of NOS activity. It inhibits NOS-I and NOS-II with Ki values of 50 Mand 78 M, respectively3. Aprotini

6、n significantly inhibits fibrinolysis with an IC50 of 0.160.05 M4.體內(nèi)研究 High dose aprotinin can reduce blood loss and transfusion requirements associated with primary cardiac proceduressuch as coronary artery bypass graft (CABG) or heart valve replacement surgery5. Aprotinin inhibits thrombusformatio

7、n in a dose-dependent manner. Aprotinin at a dose of 1.5 mg kg-1 (bolus) and 3 mg kg-1 h-1 infusion(maintenance infusion) causes a tendency towards a reduction in bleeding time. Aprotinin significantly reduces thebleeding time starting at a dose of 3 mg kg-1 bolus plus 6 mg kg-1 h-1 showing a reduct

8、ion of approximately84%2.9%. At the highest dose of 5 mg kg-1 and 10 mg kg-1 h-1, the strongest effects are observed4. Aprotinin mayaffect tumor necrosis factor-alpha (TNF) levels. Soluble TNFRI levels are significantly increased following I/R in theaprotinin treated wild type mice and not detected

9、in all TNFRInull mice6.PROTOCOLAnimal Rats: Male Wistar rats (180-220 g) are used in the study. Aprotinin is dissolved in physiological saline. Aprotinin isAdministration 46 administered by bolus injection followed by a maintenance infusion. The doses given are 1.5 mg kg-1 and 3 mg kg-1h-1, 3mg kg-1

10、 and 6 mg kg-1 h-1 up to 5 mg kg-1 and 10 mg kg-1 h-1. Plasma concentrations for the two agents areassessed by pharmacokinetic studies in rats4.Mice: An intact mouse model of ischemia/reperfusion (30 min-I/60 min-R) is used and left ventricular peak + dP/dt ismeasured in wild type mice (WT, C57BL/6;

11、 n=10), WT mice with aprotinin (4mL/kg; n=10), transgenic mice devoid ofthe TNFRI (TNFRInull; n=10), and TNFRInull with aprotinin (n=10)6.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Am J Physiol Cell Physiol. 2017 Dec 1;313(6):C632-C643.

12、 Int J Oncol. 2019 Jul;55(1):331-339.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94.2. Levy JH, et al. Efficacy and safe

13、ty of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.3. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity.Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-54. Sperzel M, et al. Evaluation of aprotinin and tranexamic acid in different in

14、 vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. JThromb Haemost. 2007 Oct;5(10):2113-8. Epub 2007 Jul 31.5. Davis R, et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995Jun;49(6):954-83.6. Sabbagh MJ, et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. JPage 2 of 3 www.MedChemECardiovasc Pharmacol. 2008 Oct;52(4):355-62.M